Bufotalin

Name: Bufotalin
Brand: MedChemExpress
SKU: HY-N0878
Rating: 5.0 (4 reviews)

Cat. No.: HY-N0878 Purity: 99.68%: FAQs
Data Sheet SDS COA Handling Instructions

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Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation.

For research use only. We do not sell to patients.

Bufotalin Chemical Structure

CAS No. : 471-95-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE Bufotalin

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.9 μM Compound: 9	Cytotoxicity against human A549 cells after 24 hrs by MTT assay Cytotoxicity against human A549 cells after 24 hrs by MTT assay	[PMID: 24050254]
A549	IC₅₀	14 nM Compound: 2a	Cytotoxicity against human A549 cells after 3 days by MTT assay Cytotoxicity against human A549 cells after 3 days by MTT assay	[PMID: 23706005]
B16-F10	IC₅₀	> 10000 nM Compound: 2a	Cytotoxicity against mouse B16F10 cells after 3 days by MTT assay Cytotoxicity against mouse B16F10 cells after 3 days by MTT assay	[PMID: 23706005]
CT26.WT	IC₅₀	> 10000 nM Compound: 2a	Cytotoxicity against mouse CT26.WT cells after 3 days by MTT assay Cytotoxicity against mouse CT26.WT cells after 3 days by MTT assay	[PMID: 23706005]
HepG2	IC₅₀	0.5 μM Compound: 9	Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay	[PMID: 24050254]
HL-60	IC₅₀	< 0.01 μg/mL Compound: 17	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 11575946]
Hs 683	IC₅₀	9 nM Compound: 2a	Cytotoxicity against human Hs683 cells after 3 days by MTT assay Cytotoxicity against human Hs683 cells after 3 days by MTT assay	[PMID: 23706005]
KB	IC₅₀	0.19 μg/mL Compound: 17	Cytotoxicity against human KB cells after 72 hrs by MTT assay Cytotoxicity against human KB cells after 72 hrs by MTT assay	[PMID: 11575946]
MCF7	IC₅₀	37 nM Compound: 2a	Cytotoxicity against human MCF7 cells after 3 days by MTT assay Cytotoxicity against human MCF7 cells after 3 days by MTT assay	[PMID: 23706005]
MH60	IC₅₀	> 25 μg/mL Compound: 17	Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay	[PMID: 11575946]
MH60	IC₅₀	> 56.2 μM Compound: 7	Growth inhibition of IL-6-independent mouse MH60 cells after 72 hrs by MTT assay Growth inhibition of IL-6-independent mouse MH60 cells after 72 hrs by MTT assay	[PMID: 15620253]
MH60	IC₅₀	> 56.2 μM Compound: 7	Growth inhibition of IL6-dependent mouse MH60 cells after 72 hrs by MTT assay in presence of human recombinant IL6 Growth inhibition of IL6-dependent mouse MH60 cells after 72 hrs by MTT assay in presence of human recombinant IL6	[PMID: 15620253]
PC-3	IC₅₀	34 nM Compound: 2a	Cytotoxicity against human PC3 cells after 3 days by MTT assay Cytotoxicity against human PC3 cells after 3 days by MTT assay	[PMID: 23706005]
SK-MEL-28	IC₅₀	65 nM Compound: 2a	Cytotoxicity against human SK-MEL-28 cells after 3 days by MTT assay Cytotoxicity against human SK-MEL-28 cells after 3 days by MTT assay	[PMID: 23706005]
U-373MG ATCC	IC₅₀	74 nM Compound: 2a	Cytotoxicity against human U373 cells after 3 days by MTT assay Cytotoxicity against human U373 cells after 3 days by MTT assay	[PMID: 23706005]

In Vitro

Bufotalin (0.1-2.5 μM; 12-96 hours) treatment dose- and time-dependently inhibits MG-63 osteoblastoma cell survival^[1].
Bufotalin (0.5-2.5 μM; 48 hours) treatment dose-dependently increases the percentage of Annexin V positive cells (apoptotic cells) and caspase-12 activity in MG-63 cells. Bufotalin-induced osteoblastoma cell apoptosis is associated with caspase-12 activation^[1].
Bufotalin (0.5-2.5 μM; 12 hours) treatment dose-dependently induces C/EBP homologous protein (CHOP) expression as well as PERK and IRE1 phosphorylation in MG-63 cells. Bufotalin induces endoplasmic reticulum (ER) stress activation in cells^[1].
Bufotalin treatment induces cell cycle arrest at G2/M phase through down-regulation of Aurora A, CDC25, CDK1, cyclin A and cyclin B1, as well as up-regulation of p53 and p21 in HepG2 cells. Bufotalin treatment also induces apoptosis which was accompanied by decrease in mitochondrial membrane potential, increases in intracellular calcium level and reactive oxygen species production, activations of caspase-9 and -3, cleavage of poly ADP-ribose polymerase (PARP) as well as changes in the expressions of bcl-2 and bax^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	MG-63 osteoblastoma cells
Concentration:	0.1 μM, 0.5 μM, 1 μM, 2.5 μM
Incubation Time:	12 hours, 24 hours, 48 hours, 72 hours, 96 hours
Result:	Inhibited MG-63 osteoblastoma cell survival.

Apoptosis Analysis^[1]

Cell Line:	MG-63 cells
Concentration:	0.5 μM, 1 μM, 2.5 μM
Incubation Time:	48 hours
Result:	Dose-dependently increased the percentage of Annexin V positive cells (apoptotic cells) and caspase-12 activity in MG-63 cells.

Western Blot Analysis^[1]

Cell Line:	MG-63 cells
Concentration:	0.5 μM, 1 μM, 2.5 μM
Incubation Time:	12 hours
Result:	Dose-dependently induced CHOP expression as well as PERK and IRE1 phosphorylation in MG-63 cells.

In Vivo

Bufotalin (0.5-1 mg/kg; intraperitoneal injection; twice daily; for 7 days) treatment shows a significantly reduced tumor growth in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SCID male mice (4-6 weeks old) injected with U2OS cells^[1]
Dosage:	0.5 mg/kg, 1 mg/kg
Administration:	Intraperitoneal injection; twice daily; for 7 days
Result:	Inhibited U2OS osteoblastoma cell growth in mice.

Molecular Weight

444.56

Formula

C₂₆H₃₆O₆

CAS No.

471-95-4

Appearance

Solid

Color

White to off-white

SMILES

C[C@@]1(CC[C@@]2([H])[C@@]3([H])CC[C@@]4([H])[C@@]2(CC[C@H](O)C4)C)[C@@H](C(C=C5)=COC5=O)[C@@H](OC(C)=O)C[C@@]13O

Structure Classification

Steroids

Initial Source

Animals

toad

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (224.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2494 mL	11.2471 mL	22.4942 mL
5 mM	0.4499 mL	2.2494 mL	4.4988 mL
10 mM	0.2249 mL	1.1247 mL	2.2494 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.68%

Select Batch:

Data Sheet (281 KB) SDS (480 KB)

COA (252 KB) HNMR (281 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Zhu YR, et al. Bufotalin-induced apoptosis in osteoblastoma cells is associated with endoplasmic reticulum stress activation. Biochem Biophys Res Commun. 2014 Aug 15;451(1):112-8. [Content Brief]

[2]. Zhang DM, et al. Bufotalin from Venenum Bufonis inhibits growth of multidrug resistant HepG2 cells through G2/M cell cycle arrest and apoptosis. Eur J Pharmacol. 2012 Oct 5;692(1-3):19-28. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2494 mL	11.2471 mL	22.4942 mL	56.2354 mL
	5 mM	0.4499 mL	2.2494 mL	4.4988 mL	11.2471 mL
	10 mM	0.2249 mL	1.1247 mL	2.2494 mL	5.6235 mL
	15 mM	0.1500 mL	0.7498 mL	1.4996 mL	3.7490 mL
	20 mM	0.1125 mL	0.5624 mL	1.1247 mL	2.8118 mL
	25 mM	0.0900 mL	0.4499 mL	0.8998 mL	2.2494 mL
	30 mM	0.0750 mL	0.3749 mL	0.7498 mL	1.8745 mL
	40 mM	0.0562 mL	0.2812 mL	0.5624 mL	1.4059 mL
	50 mM	0.0450 mL	0.2249 mL	0.4499 mL	1.1247 mL
	60 mM	0.0375 mL	0.1875 mL	0.3749 mL	0.9373 mL
	80 mM	0.0281 mL	0.1406 mL	0.2812 mL	0.7029 mL
	100 mM	0.0225 mL	0.1125 mL	0.2249 mL	0.5624 mL

Bufotalin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bufotalin471-95-4ApoptosisReactive Oxygen SpeciesCHOPendoplasmicreticulumPERKIRE1caspase-12antitumorInhibitorinhibitorinhibit

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Bufotalin

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Bufotalin Related Antibodies

4 Publications Citing Use of MCE Bufotalin

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Complete Stock Solution Preparation Table

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